BIIE0246

Antagonist of NPY2R

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe BIIE0246 is in the process of SERP review.

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Information

NPY2R

Antagonist

up to 1 uM

More...

Probe Availability:

In Vitro Validations

Uniprot ID: P49146

Target Class: GPCR

Target SubClass: Neuropeptide Y receptor Y2

PDB ID for probe-target interaction (3D structure): --

Structure-activity relationship: no

Target aliases:

Neuropeptide Y receptor type 2, NPY2R, NPY2R_HUMAN ...

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Cell:

Selectivity vs family members was assessed on rat homologs using radioligand binding assay in HEK293T cells expressing respective receptor: rY2R 15 nM, rY1R, rY4R and rY5R >10 uM IC50; no cross-reactivity with 60 other receptors.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

For in vivo CNS studies inject intrathecally or directly in region of interest.

(last updated: 7 Jul 2021 )

SERP+ Ratings

In Cell Rating

In Model Organisms

SERP+ Comments:

Consult opnME (Boehringer Ingelheim) for further in depth ADME and selectivity data. Due to the poor reported solubility, permeability, moderate metabolic stability (and PPB), BIIE0246 is not recommended as an in vivo probe for NPY2R unless dosed intrathecally. Other selective probes for NPY2R are available, detailed in the pdf available from the opnME website.

(last updated: 14 Oct 2025 )